Methods of reversing ticagrelor activity
AssigneeSFJ Pharmaceutical X, LTD.
InventorsJohn Lee, David James Ballance
Life of this patent
Estimating the term…
Abstract
The present disclosure provides a method of reversing ticagrelor-associated bleeding in a patient by administering an antibody or fragment thereof that binds to ticagrelor.
Claims40
A method of reversing ticagrelor-associated bleeding, or reducing the risk of said bleeding, in a patient who had previously been administered ticagrelor, comprising administering to the patient a pharmaceutical composition comprising a dose of between about 18 g and about 48 g of an antibody or fragment thereof that binds to ticagrelor ((1S,2S,3R,5S)-3-[7-{[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol) or a metabolite or derivative thereof,
- wherein the antibody or fragment thereof comprises complementarity-determining region (CDR) combinations selected from the group consisting of:
- a) SEQ ID NO:53 (VH CDR1), SEQ ID NO:54 (VH CDR2), SEQ ID NO:55 (VH CDR3), SEQ ID NO:58 (VL CDR1), SEQ ID NO:59 (VL CDR2), and SEQ ID NO:60 (VL CDR3);
- b) SEQ ID NO:63 (VH CDR1), SEQ ID NO:64 (VH CDR2), SEQ ID NO:65 (VH CDR3), SEQ ID NO:68 (VL CDR1), SEQ ID NO:69 (VL CDR2), and SEQ ID NO:70 (VL CDR3);
- and
- c) SEQ ID NO:73 (VH CDR1), SEQ ID NO:74 (VH CDR2), SEQ ID NO:75 (VH CDR3), SEQ ID NO:78 (VL CDR1), SEQ ID NO:79 (VL CDR2), and SEQ ID NO:80 (VL CDR3).
A method of reversing ticagrelor-associated bleeding, or reducing the risk of said bleeding, in a patient who had previously been administered ticagrelor, comprising administering to the patient a pharmaceutical composition comprising a dose of about 36 g of an antibody Fab fragment that binds to ticagrelor ((1S,2S,3R,5S)-3-[7-{[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol) or ticagrelor active metabolite (TAM),
- wherein the Fab thereof comprises complementarity-determining region (CDR) combination:
- SEQ ID NO:73 (VH CDR1), SEQ ID NO:74 (VH CDR2), SEQ ID NO:75 (VH CDR3), SEQ ID NO:78 (VL CDR1), SEQ ID NO:79 (VL CDR2), and SEQ ID NO:80 (VL CDR3);
- wherein the pharmaceutical composition is administered in the following schedule:
- 12 g of the antibody or fragment thereof infused over 10 minutes, followed by 12 g of the antibody or fragment thereof over 6 hours, followed by 12 g of the antibody or fragment thereof over 18 hours.
Dependencies are inferred from the claim text.